Medicinal Chemistry

Terry L. Carmack

Publications

• Research Article
  Synthesis, Sigma Receptor Binding Studies, and In Vivo Evaluation of Radioiodinated (Z)- and (E)-iodoallyl Analogs of SA4503
  Author(s): Rong Xu, Lisa D. Watkinson, Terry L. Carmack, John R. Lever and Susan Z. LeverRong Xu, Lisa D. Watkinson, Terry L. Carmack, John R. Lever and Susan Z. Lever
  
  SA4503, a potent σ1 receptor agonist, is under study for functional recovery after stroke, and has been tested for treatment of major depression. Recent behavioral studies indicate that SA4503 can also display antagonist properties, and attenuates psychostimulant-induced hyperactivity in animal models. Further, SA4503 labeled with carbon-11 (halflife 20.4 min), or analogs labeled with fluorine-18 (half-life 109.7 min), are useful for PET studies of the σ1 receptor. Analogs labeled with iodine-123 (13.2 h half-life) would have potential as SPECT imaging agents, while analogs labeled with iodine-125 (60.1 d half-life) could be used routinely in laboratory studies. Toward these ends, we describe the synthesis and radiolabeling, as well as in vitro and in vivo binding studies, of two SA4503 analogs where the 4-methoxy group of the dimethoxyphenethyl moiety is replaced by eithe.. Read More»
  DOI: 10.4172/2161-0444.1000128

  Abstract PDF